"目录号: HY-14291
Vildagliptin (LAF-237; NVP-LAF 237)能抑制DPP-4，IC50为2.3 nM。
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Description
Vildagliptin (LAF-237; NVP-LAF 237) inhibits DPP-4 with IC50 of 2.3 nM.IC50 Value: 2.3 nM[1]Target: DPP-4in vitro: Vildagliptin is an N-substituted glycyl-2-cyanopyrrolidine (figure 2). It is a potent competitive and reversible inhibitor of human and rodent DPP-4 in vitro, with a median inhibitory concentration (IC50) ~2-3 nmol/L. Importantly, vildagliptin inhibits DPP-4 with high specificity relative to other similar peptidases where its IC50 exceeds 200 mol/L [1].in vivo: Compared to age-, gender-, BMI-matched subjects with normal renal function, the mean AUC of vildagliptin after 14 days in patients with mild, moderate, and severe RI increased by 40%, 71%, and 100%, respectively [2]. The treatment was effective in modulating stress in pancreatic tissue, both by reducing levels of stress markers as well as by increasing activity of SOD and catalase. After analyzing the pancreatic histology, we found that vildagliptin was also able to preserve islets and pancreatic β-cells, especially at the concentration of 5 mg/kg [3].Clinical trial: FDA approved drug.
Clinical Trial
Novartis Pharmaceuticals-Novartis
Type-2 Diabetes Mellitus
May 13, 2013
Phase 4
Mayo Clinic-Novartis Pharmaceuticals
Diabetes Mellitus, Non-Insulin-Dependent
May 2005
Phase 3
Novartis
Healthy
September 2006
Phase 1
Novartis
Healthy
December 2006
Phase 1
Novartis Pharmaceuticals-Novartis
Type 2 Diabetes Mellitus (T2DM)
December 2013
Phase 4
Novartis Pharmaceuticals-Novartis
Diabetes Mellitus, Type 2
May 2004
Phase 3
Novartis Pharmaceuticals-Novartis
Type 2 Diabetes
February 2011
Phase 4
Novartis Pharmaceuticals-Novartis
Type 2 Diabetes Mellitus
August 2012
Phase 4
Pusan National University Hospital
Type 2 Diabetes
December 2009
Phase 4
Novartis Pharmaceuticals-Novartis
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November 2012
Phase 4
Novartis Pharmaceuticals-Novartis
Diabetes Mellitus, Type 2
April 2013
Phase 4
Novartis Pharmaceuticals-Novartis
Type 2 Diabetes
February 2012
Phase 4
Lund University
Diabetes-Hypoglycemia
September 2010
Phase 4
Medical University of Vienna
Diabetes Mellitus
September 2009
Phase 2
Rio de Janeiro State University-Laboratory for Clinical and Experimental Research on Vascular Biology
1- Microvascular Function-2-oxidative Stress-3-inflammation
April 2013
Phase 4
Novartis Pharmaceuticals-Novartis
Type 2 Diabetes Mellitus
October 2010
Phase 4
Dr. José Fernando Vilela-Martin MD PhD-Novartis-Hospital de Base
Type 2 Diabetes Mellitus-Hypertension-Endothelial Dysfunction
July 2013
Phase 4
Lund University
Diabetes
January 2012
Phase 4
Johann Wolfgang Goethe University Hospital
SDF-1 is an Important Cytokine for Neovascularization. Cleavage of SDF-1 is Reduced by DPPIV Inhibitors
July 2009
Phase 2-Phase 3
Novartis
Diabetes Mellitus, Type 2
February 2008
Phase 1-Phase 2
Novartis Pharmaceuticals-Novartis
Type 2 Diabetes Mellitus
April 2012
Phase 3
Novartis Pharmaceuticals-Novartis
Type 2 Diabetes Mellitus
December 2010
Phase 3
Novartis
Diabetes Mellitus, Type 2
January 2006
Phase 3
Novartis Pharmaceuticals-Novartis
Diabetes Mellitus, Type 2
December 2011
Phase 3
Novartis Pharmaceuticals-Novartis
Diabetes Mellitus, Type 2
May 2004
Phase 3
Novartis Pharmaceuticals-Novartis
Diabetes Mellitus Type 2
June 2011
Phase 4
Seoul National University Bundang Hospital
Diabetes
January 2010
Phase 4
Federal University of São Paulo-Novartis
Type 1 Diabetes-Insulin Dependent Diabetes-Juvenile Onset Diabetes Mellitus-Autoimmune Diabetes
March 2014
Phase 3
Novartis
Diabetes Mellitus, Type 2
November 2004
Phase 3
Novartis Pharmaceuticals-Novartis
Diabetes Mellitus, Type 2
October 2004
Phase 3
Lund University
Type 2 Diabetes
January 2016
Phase 4
Novartis Pharmaceuticals-Novartis
Congestive Heart Failure-Type II Diabetes Mellitus
May 2009
Phase 4
Novartis Pharmaceuticals-Novartis
Type 2 Diabetes Mellitus
March 30, 2012
Phase 4
Novartis Pharmaceuticals-Novartis
Diabetes Mellitus, Type 2
January 2004
Phase 3
Novartis Pharmaceuticals-Novartis
Diabetes Mellitus, Type 2
October 2006
Phase 3
Genuine Research Center, Egypt-EVA pharma, Egypt
Healthy
February 2014
Phase 1
Novartis
Type-2 Diabetes
July 2007
Phase 1
Radboud University
Type 2 Diabetes-Endothelial Dysfunction
January 2010
Phase 3
Novartis
Diabetes Mellitus, Type 2
January 2006
Phase 3
Novartis Pharmaceuticals-Novartis
Type 2 Diabetes Mellitus
January 2013
Phase 4
Novartis
Diabetes Mellitus, Type 2
January 2008
Phase 3
Novartis
Type 2 Diabetes Mellitus
October 2010
Phase 3
Novartis
Diabetes Mellitus, Type 2-Renal Insufficiency
September 2008
Phase 3
Novartis
Type 2 Diabetes Mellitus
March 2010
Phase 4
Novartis
Diabetes Mellitus, Type 2
October 2004
Phase 3
Novartis Pharmaceuticals-Novartis
Type II Diabetes Mellitus
November 2010
Phase 3
Novartis
Diabetes Mellitus, Type 2
January 2005
Phase 3
Novartis Pharmaceuticals-Novartis
Type 2 Diabetes
June 2010
Phase 3
Novartis Pharmaceuticals-Novartis
Type 2 Diabetes Mellitus
April 2011
Phase 3
Azienda Ospedaliero-Universitaria di Parma
Type 2
